85-2076-33　REV-ERB Agonist II, SR9009 25mg　CAS No:1379686-30-2　217739

特徴

• A pyrrolidinecarbamate compound that acts as a specific REV-ERB-alpha/beta agonist. Exhibits a direct and reversible binding (Kd = 800nM REV-ERB-alpha) and shows excellent selectivity over a panel of 46 other nuclear receptors. Potently increases REV-ERB-dependent repressor activity (IC50 = 670 and 800nM in Gal4-REV-ERB-alpha and beta transfected HEK 293 cells) and reduces BMAL1 mRNA in HepG2 cells (IC50 = 710nM). Shown to cross the blood-brain barrier and exhibit desirable pharmacokinetic properties. A 7-day administration of SR9009 (100mg/kg, i.p., b.i.d.) causes a significant weight and fat loss in C57BL6 mice with concomitant reduction in plasma glucose and free fatty acid levels, and alters circadian pattern.
• 217739, CAS # 1379686-30-2, acts as a specific REV-ERB-α/β agonist that exhibits a direct and reversible binding (Kd = 800nM).
• Synonyms:Ethyl-3-(((4-chlorobenzyl)((5-nitrothiophen-2-yl)methyl)amino)methyl)pyrrolidine-1-carboxylate
• Molecular Weight:437.9
• Molecular Formula:C₂₀H₂₄ClN₃O₄S
• Solubility:DMSO
• Primary Target:REV-ERB-alpha/beta
• Appearance:Dark brown liquid.
• Purity:≥96% (HPLC)
• Storage and Stability:Store at 4°C under inert atmosphere. For maximum recovery of product, centrifuge the original vial prior to removing the cap.